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Antimicrob Agents Chemother ; 55(1): 311-20, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-20937782

RESUMO

Screening of various bisquaternary bisnaphthalimides against a variety of human pathogens revealed one compound, designated MT02, with strong inhibitory effects against Gram-positive bacteria. The MICs ranged from 0.31 µg/ml against community-acquired methicillin-resistant Staphylococcus aureus (MRSA) lineage USA300 to 20 µg/ml against Streptococcus pneumoniae. Radioactive whole-cell labeling experiments indicated a strong impact of MT02 on bacterial DNA replication. DNA microarray studies generated a transcriptional signature characterized by stronger expression of genes involved in DNA metabolism, DNA replication, SOS response, and transport of positively charged compounds. Furthermore, surface plasmon resonance and gel retardation experiments demonstrated direct binding of MT02 to DNA in a concentration-dependent, reversible, and non-sequence-specific manner. The data presented suggest that the bisquaternary bisnaphthalimide MT02 exerts anti-Gram-positive activity by binding to DNA and thereby preventing appropriate DNA replication.


Assuntos
Antibacterianos/farmacologia , Proteínas de Bactérias/efeitos dos fármacos , Substâncias Intercalantes/farmacologia , Antibacterianos/química , Proteínas de Bactérias/genética , Linhagem Celular , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Substâncias Intercalantes/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Análise de Sequência com Séries de Oligonucleotídeos , Staphylococcus aureus/genética
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